CAS: 185315-48-4; (4-Bromo-2-Chlorophenyl)Methanol

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CAS号59748-90-2 4-溴-2-氯苯甲酸 | CAS号185312-82-7 2-氯-4-溴苯甲酸甲酯 | CAS号158435-41-7 4-溴-2-氯苯甲醛 | CAS号916516-89-7 2-(4-溴-2-氯苯基)乙酸 | CAS号21924-83-4 4-溴甲基-3-氯苯腈 | CAS号89720-77-4 2-氯-4-溴溴苄 | CAS号1261606-45-4 4-Bromo-2-chlor... | CAS号158435-41-7 4-溴-2-氯苯甲醛 | CAS号67197-54-0 2-氯-4-溴苯基乙腈

4-溴-2-氯甲苯置于盐酸,Potassium Permanganate,锂硼氢体系中,用 四氢呋喃,甲醇,水,叔丁醇 用作溶剂,化学反应 12.0H,反应生成4-溴-2-氯苄醇
参考文献:Stilbene Boronic Acids Form A Covalent Bond With Human Transthyretin And Inhibit Its Aggregation
标题:Stilbene Boronic Acids Form A Covalent Bond With Human Transthyretin And Inhibit Its Aggregation
摘要:Transthyretin (Ttr) Is A Homotetrameric Protein. Its Dissociation Into Monomers Leads To The Formation Of Fibrils That Underlie Human Amyloidogenic Diseases. The Binding Of Small Molecules To The Thyroxin-Binding Sites In Ttr Stabilizes The Homotetramer And Attenuates Ttr Amyloidosis. Herein,We Report On Boronic Acid-Substituted Stilbenes That Limit Ttr Amyloidosis In Vitro. Assays Of Affinity For Ttr And Inhibition Of Its Tendency To Form Fibrils Were Coupled With X-Ray Crystallographic Analysis Of Nine Ttr. Ligand Complexes. The Ensuing Structure-Function Data Led To A Symmetrical Diboronic Acid That Forms A Boronic Ester Reversibly With Serine 117. This Diboronic Acid Inhibits Fibril Formation By Both Wild-Type Ttr And A Common Disease Related Variant,V30M Ttr,As Effectively As Does Tafamidis,A Small-Molecule Drug Used To Treat Ttr-Related Amyloidosis In The Clinic. These Findings Establish A New Modality For Covalent Inhibition Of Fibril Formation And Illuminate A Path For Future Optimization.
Doi:10.1021/acs.Jmedchem.7B00952